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Assay Detail

CHEMBL1016090

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Functional
Inhibition of fetal calf serum-induced proliferation of human foreskin fibroblast assessed as [3H]thymidine incorporation after 4 days by scintillation counting
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type HFF
Confidence 1 — Organism
Curated By Autocuration

Target

HFF (CHEMBL614071)
Type CELL-LINE
Organism Homo sapiens

Publication

Prevention of organ allograft rejection by a specific Janus kinase 3 inhibitor.
Changelian PS, Flanagan ME, Ball DJ, Kent CR, Magnuson KS, Martin WH, Rizzuti BJ, Sawyer PS, Perry BD, Brissette WH, McCurdy SP, Kudlacz EM, Conklyn MJ, Elliott EA, Koslov ER, Fisher MB, Strelevitz TJ, Yoon K, Whipple DA, Sun J, Munchhof MJ, Doty JL, Casavant JM, Blumenkopf TA, Hines M, Brown MF, Lillie BM, Subramanyam C, Shang-Poa C, Milici AJ, Beckius GE, Moyer JD, Su C, Woodworth TG, Gaweco AS, Beals CR, Littman BH, Fisher DA, Smith JF, Zagouras P, Magna HA, Saltarelli MJ, Johnson KS, Nelms LF, Des Etages SG, Hayes LS, Kawabata TT, Finco-Kent D, Baker DL, Larson M, Si MS, Paniagua R, Higgins J, Holm B, Reitz B, Zhou YJ, Morris RE, O'Shea JJ, Borie DC.
Science (2003) 302 : 875 -878
PubMed 14593182 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 5.15 5.25

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL56543 1 5.25
CHEMBL473773 1 5.20
CHEMBL463821 1 5.00
CHEMBL405130 WHI-P131 1.0 1 -
CHEMBL221959 TOFACITINIB 4.0 1 -
CHEMBL160 CYCLOSPORINE 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL56543 IC50 = 5584.0 nM 5.25
CHEMBL473773 IC50 = 6343.0 nM 5.20
CHEMBL463821 IC50 = 10000.0 nM 5.00
CHEMBL405130 WHI-P131 IC50 - -
CHEMBL221959 TOFACITINIB IC50 > 10000.0 nM -
CHEMBL160 CYCLOSPORINE IC50 > 10000.0 nM -